Abstract
Results: Basic physicochemical properties including their apparent solubility in aqueous buffer and vegetable oils of a series of 11 peptidomimetics varying with respect to chain length and degree of N-methylation were estimated. It was observed that the compounds in contact with water transformed into sticky, slowly dissolving semisolid materials. Based on these observations, the in vitro release behavior of selected peptide derivatives from oil solutions and in situ formed precipitates was investigated using a validated in vitro release model. Conclusion: The results of this investigation suggest that both types of oil-based drug delivery systems might constitute alternative sustained release formulation principles of such amorphous peptide derivatives for the intra-articular route of administration.
Acknowledgments
The present study was supported by Novo Nordisk A/S via the Drug Research Academy, Faculty of Pharmaceutical Sciences, University of Copenhagen, Denmark, The Danish Medical Research Council, and the Danish Rheumatism Association. The technical assistance of Peter Andersen (Novo Nordisk A/S) during synthesis of the peptidomimetics is highly valued.
Declaration of interest
The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this paper.